|Solubility:||DMSO up to 100 mM|
|Chemical Name:||ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
GSK-J4 is an ethyl ester derivative of GSK-J1, which is the first selective and potent inhibitor of the H3K27 histone demethylases UTX and JMJD3. The highly polar carboxylate group of GSK-J1 restricts its cellular permeability, therefore GSK-J4 was developed as a pro-drug, masking the polarity of the acid group of the GSK-J1, for cellular assays. GSK-J4 could significant reduce LPS-induced pro-inflammatory cytokine production in primary human macrophages (IC50 ~9 μM for the inhibition of TNFα release). Together with GSK-J1, GSK-J4 could be a unique small molecule to allow selective pharmacological intervention across the JMJ family.
How to Use:
- In vitro: GSK-J4 was used at 30 µM final concentration in cellular assays.
- In vivo: n/a
- 1. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response (2012) Nature. 488(7411):404-8.
- 2. SGC website: http://www.thesgc.org/scientists/chemical_probes/GSKJ1
Products are for research use only. Not for human use.
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